title: Malvidin-3-O-β glucoside, major grape anthocyanin, inhibits human macrophage-derived inflammatory mediators and decreases clinical scores in arthritic rats.
abstract: Polyphenolic anthocyanins are major colorful compounds in red fruits, known to prevent cardiovascular and other diseases. Grape polyphenols are a mixture of various molecules and their exact contribution to above bioactivities remains to be clarified. In the present study, we first analyzed the effect of purified grape-derived compounds on human peripheral blood mononuclear cell (PBMC) survival, proliferation, as well as for their ability to inhibit the activation of human normal macrophages. Data indicated that malvidin-3-O-β glucoside (Malβg), the major grape anthocyanin, is bioactive with no toxicity on human PBMC. Malβg decreased the transcription of genes encoding inflammatory mediators, confirmed by the inhibition of TNFα, IL1, IL-6 and iNOS-derived nitric oxide (NO) secretion from activated macrophages. As Malβg also inhibited inflammatory response of rat macrophages, we investigated the anti-inflammatory potential of Malβg in chronic rat adjuvant-induced arthritis (AIA). Malβg significantly diminished inflammatory cachexia and arthritic paw scores in AIA rats at both therapeutic and preventive levels. In vivo effects of Malβg correlated with down-regulation of NO generation from AIA rats' peritoneal macrophages ex vivo. These data indicate that Malβg, major grape anthocyanin, is a potent anti-inflammatory agent in vitro and in vivo, without detectable toxic effect.
authors.affiliation: Study Group of Biologically Active Plant Substances, EA3675, Faculty of Pharmacy, Bordeaux Segalen University, France.
authors.forename: Alain
authors.initials: A
authors.lastname: Decendit
authors.forename: Maria
authors.initials: M
authors.lastname: Mamani-Matsuda
authors.forename: Virginie
authors.initials: V
authors.lastname: Aumont
authors.forename: Pierre
authors.initials: P
authors.lastname: Waffo-Teguo
authors.forename: Daniel
authors.initials: D
authors.lastname: Moynet
authors.forename: Katia
authors.initials: K
authors.lastname: Boniface
authors.forename: Emmanuel
authors.initials: E
authors.lastname: Richard
authors.forename: Stéphanie
authors.initials: S
authors.lastname: Krisa
authors.forename: Jérôme
authors.initials: J
authors.lastname: Rambert
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Mérillon
authors.forename: M D
authors.initials: MD
authors.lastname: Mossalayi
mesh_terms: D000818:Animals; D000872:Anthocyanins / Q000494:pharmacology* / Q000627:therapeutic use; D000893:Anti-Inflammatory Agents / Q000494:pharmacology* / Q000627:therapeutic use; D001169:Arthritis, Experimental / Q000188:drug therapy* / Q000378:metabolism / Q000503:physiopathology; D002908:Chronic Disease; D016207:Cytokines / Q000037:antagonists & inhibitors* / Q000378:metabolism; D005260:Female; D005960:Glucosides / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D007375:Interleukin-1 / Q000037:antagonists & inhibitors / Q000378:metabolism; D015850:Interleukin-6 / Q000378:metabolism; D007963:Leukocytes, Mononuclear / Q000187:drug effects / Q000378:metabolism; D008262:Macrophage Activation; D017737:Macrophages, Peritoneal / Q000187:drug effects* / Q000378:metabolism; D009569:Nitric Oxide / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D052247:Nitric Oxide Synthase Type II / Q000037:antagonists & inhibitors / Q000378:metabolism; D059808:Polyphenols / Q000494:pharmacology; D051381:Rats; D011917:Rats, Inbred Lew; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000378:metabolism; D027843:Vitis; D000093242:Interleukin-6 Inhibitors
chemical_list: D000872:Anthocyanins; D000893:Anti-Inflammatory Agents; D016207:Cytokines; D005960:Glucosides; D007375:Interleukin-1; D015850:Interleukin-6; D009569:Nitric Oxide; D052247:Nitric Oxide Synthase Type II; D059808:Polyphenols; D014409:Tumor Necrosis Factor-alpha; D000093242:Interleukin-6 Inhibitors; C458419:malvidin-3-glucoside
keywords: AIA; Arthritis; HC; Inflammation; LPS; MDM; MIP1α; Macrophage; Malvidin-3-O-β glucoside; Malβg; NO; NO synthase; NOS; PBL; PBMC; RA; TNF; adjuvant-induced arthritis; hydrocortisone; lipopolysaccharides; macrophage inflammatory protein 1α; malvidin-3-O-β glucoside; monocyte-derived macrophages; nitric oxide; peripheral blood leukocytes; peripheral blood mononuclear cells; rheumatoid arthritis; tumor necrosis factor